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AG 555 Sale

(Synonyms: Tyrphostin AG 555) 目录号 : GC11744

A tyrphostin EGFR inhibitor

AG 555 Chemical Structure

Cas No.:133550-34-2

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10mg
¥765.00
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50mg
¥3,060.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

ID13 mouse fibroblasts are maintained in Dulbecco's modified Eagle's medium supplemented with 5% (v/v) fetal calf serum, 100 units/mL Penicillin, and 100 μg/mL Streptomycin. Cells are seeded at 2.5×104 cells/cm2 to ensure logarithmic growth. The final concentration of the Tyrphostin AG 555 is 30 μM in all experiments. Stock solutions of 10 mM in Me2SO are stored at -80°C. To exclude potential Me2SO effects, the same final concentrations (0.3%) of Me2SO are added to nontreated controls. Actinomycin D is dissolved in water and added to cells in a final concentration of 5 μg/mL. SB 203580 is dissolved in Me2SO (stock concentration: 50 mM) and used in a final concentration of 10 μM[2].

References:

[1]. Michaelis M, et al. Cisplatin-resistant neuroblastoma cells express enhanced levels of epidermal growth factor receptor (EGFR) and are sensitive to treatment with EGFR-specific toxins. Clin Cancer Res. 2008 Oct 15;14(20):6531-7.
[2]. Baars S, et al. Tyrphostin AG 555 inhibits bovine papillomavirus transcription by changing the ratio between E2 transactivator/repressor function. J Biol Chem. 2003 Sep 26;278(39):37306-13.
[3]. Ben-Bassat H, et al. Tyrphostins that suppress the growth of human papilloma virus 16-immortalized human keratinocytes. J Pharmacol Exp Ther. 1999 Sep;290(3):1442-57.

产品描述

AG 555 is a potent and selective inhibitor of EGFR with IC50 value of 0.7 μM.

The epidermal growth factor receptor (EGFR) is the cell-surface receptor for epidermal growth factor and plays an important role in tumor invasion and cancer cell proliferation.

AG 555 is a potent and selective EGFR inhibitor. In HPV16-immortalized human keratinocytes, AG 555 inhibited the activation of Cdk2 and induced growth arrest at the G1 phase accompanied by 15-20% cell apoptosis [1]. AG556 arrested cells at G1/S phase by 85% and inhibited the activation of Cdk2 by phosphorylating tyrosine 15 on Cdk2 [2]. In A-498, Caki-1 and Caki-2 renal carcinoma cell lines and RT4, J82 and T24 transitional carcinoma cell lines, AG555 inhibited cell proliferation with IC50 values ranging from 3 to 16 μM in a dose-dependent way. AG555 (10-30 μM) completely inhibited cell growth [3]. In NIH/3T3 cells infected with Moloney murine leukemia virus (Mo-MuLV), AG-555 inhibited the viral DNA integrated into the host genome in acutely infected cells. While in chronically infected cells, AG-555 decreased the level of viral RNA and inhibited viral protein synthesis [4].

References:
[1].  Ben-Bassat H, Rosenbaum-Mitrani S, Hartzstark Z, et al. Inhibitors of epidermal growth factor receptor kinase and of cyclin-dependent kinase 2 activation induce growth arrest, differentiation, and apoptosis of human papilloma virus 16-immortalized human keratinocytes. Cancer Res, 1997, 57(17): 3741-3750.
[2].  Kleinberger-Doron N, Shelah N, Capone R, et al. Inhibition of Cdk2 activation by selected tyrphostins causes cell cycle arrest at late G1 and S phase. Exp Cell Res, 1998, 241(2): 340-351.
[3].  Sion-Vardy N, Vardy D, Rodeck U, et al. Antiproliferative effects of tyrosine kinase inhibitors (tyrphostins) on human bladder and renal carcinoma cells. J Surg Res, 1995, 59(6): 675-680.
[4].  Seri I, Aflalo E, Gazit A, et al. Tyrphostin AG-555 inhibits early and late stages of Moloney murine leukemia virus replication cycle. Int J Oncol, 1997, 10(6): 1185-1189.

Chemical Properties

Cas No. 133550-34-2 SDF
别名 Tyrphostin AG 555
化学名 (E)-2-cyano-3-(3,4-dihydroxyphenyl)-N-(3-phenylpropyl)acrylamide
Canonical SMILES O=C(/C(C#N)=C/C(C=C1O)=CC=C1O)NCCCC2=CC=CC=C2
分子式 C19H18N2O3 分子量 322.36
溶解度 DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml,Ethanol: 20 mg/ml 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mg 5 mg 10 mg
1 mM 3.1021 mL 15.5106 mL 31.0212 mL
5 mM 0.6204 mL 3.1021 mL 6.2042 mL
10 mM 0.3102 mL 1.5511 mL 3.1021 mL
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